11β-hydroxysteroid dehydrogenase-1 as a therapeutic target for metabolic diseases

被引:43
作者
Fotsch, C [1 ]
Askew, BC [1 ]
Chen, JJ [1 ]
机构
[1] Amgen Inc, Chem Res & Discovery, Thousand Oaks, CA 91320 USA
关键词
11 beta-hydroxysteroid dehydrogenase (11 beta HSD1); diabetes; gluconeogenesis; hydroxysteroid dehydrogenase; inhibitor;
D O I
10.1517/13543776.15.3.289
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
11 beta-Hydroxysteroid dehydrogenase-1 (11 beta HSD1) is a therapeutic target for Type 2 diabetes that has stimulated the interest of many pharmaceutical companies. Mounting evidence obtained from both preclinical and clinical studies support the contention that inhibiting 11 beta HSD1 will have a therapeutic benefit by lowering glucose output and increasing insulin sensitivity. In just over two years, 21 applications containing 11 beta HSD1 inhibitors have been published. In this review, the target rationale and patent applications from Merck, Novo Nordisk, AstraZeneca, Sterix, Biovitrum, Janssen and Novartis will be discussed.
引用
收藏
页码:289 / 303
页数:15
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